Karo Bio Ab

Ye Liu

Minsheng Zhang

Johan Malm

Yi-Lin Li

Denis E Ryono

Jon J Hangeland

Konrad Koehler

Yolanda V Caringal

Neeraj Garg

Chris Litten

Ana Maria Garcia Collazo

Asa Hedfors

Charlotta Mellin

New thyroid receptor ligands are provided which have general formula (I) in which: n is an integer from 0 to 4; Ris halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; Rand Rare the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 5 carbons, at least one of Rand Rbeing other than hydrogen; Ris a carboxylic acid amide (CONR'R&#x2033;) or an acylsulphonamide (CONHSOR&#x2032;) derivative, or a pharmaceutically acceptable salt thereof, and all stereolsom thereof; or when n is equal to or greater than one, Rmay be heteroaromatic moiety which may be substituted or unsubstituted, or an amine (NR&#x2032;R&#x2033;). Ris hydrogen or an acyl (such as acetyl or benzoyl) or other group capable of bioconversion to generate the free phenol structure (wherein R&#x2014;H). In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependant upon the expression of a Tregulated gene, wherein a compound as described above is administered in a therapeutically effective amount. Examples of such diseases associated with metabolism dysfunction or are dependent upon the expression of a Tregulated gene include obesity, hypercholesterolemia, atherosclerosis, cardiac arrhythmias, depression, osteoporosis, hypothyroidism, goiter, thyroid cancer as well as glaucoma, congestive heart failure and skin disorders. 

Thyroid receptor ligands and method II

New thyroid receptor ligands are provided which have general formula (I) in which: n is an integer from 0 to 4; Ris halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; Rand Rare the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 5 carbons, at least one of Rand Rbeing other than hydrogen; Ris a carboxylic acid amide (CONR'R&#x2033;) or an acylsulphonamide (CONHSO2R&#x2032;) derivative, or a pharmaceutically acceptable salt thereof, and all stereoisomers thereof; or when n is equal to or greater than one, Rmay be a heteroaromatic moiety which may be substituted or unsubstituted, or an amine (NR&#x2032;R&#x2033;). Ris hydrogen or an acyl (such as acetyl or benzoyl) or other group capable of bioconversion to generate the free phenol structure (wherein R=H). In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependent upon the expression of a Tregulated gene, wherein a compound as described above is administered in a therapeutically effective amount. Examples of such diseases associated with metabolism dysfunction or are dependent upon the expression of a Tregulated gene include obesity, hypercholesterolemia, atherosclerosis, cardiac arrhythmias, depression, osteoporosis, hypothyroidism, goiter, thyroid cancer as well as glaucoma, congestive heart failure and skin disorders.

Thyroid receptor ligands and method

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Tullinge, Sweden

Ye Liu